Synthesis of febrifugine derivatives and development of an effective and safe tetrahydroquinazoline-type antimalarial

Haruhisa Kikuchi, Seiko Horoiwa, Ryota Kasahara, Norimitsu Hariguchi, Makoto Matsumoto, Yoshiteru Oshima

Research output: Contribution to journalArticlepeer-review

32 Citations (Scopus)

Abstract

Febrifugine, a quinazoline alkaloid isolated from Dichroa febrifuga roots, shows powerful antimalarial activity against Plasmodium falciparum. Although the use of ferifugine as an antimalarial drug has been precluded because of its severe side effects, its potent antimalarial activity has stimulated medicinal chemists to pursue its derivatives instead, which may provide valuable leads for novel antimalarial drugs. In the present study, we synthesized new derivatives of febrifugine and evaluated their in vitro and in vivo antimalarial activities to develop antimalarials that are more effective and safer. As a result, we proposed tetrahydroquinazoline-type derivative as a safe and effective antimalarial candidate.

Original languageEnglish
Pages (from-to)10-19
Number of pages10
JournalEuropean Journal of Medicinal Chemistry
Volume76
DOIs
Publication statusPublished - 2014 Apr 9
Externally publishedYes

Keywords

  • Antimalarials
  • Plasmodium falciparum
  • Quinazoline alkaloids
  • Structure-activity relationship

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Fingerprint

Dive into the research topics of 'Synthesis of febrifugine derivatives and development of an effective and safe tetrahydroquinazoline-type antimalarial'. Together they form a unique fingerprint.

Cite this